Ubiquitin-proteasome pathway is responsible for the degradation of various intracorporal tissue proteins, most of which are closely related to physiological functions, thus the pathway plays a role of regulating various cellular mechanisms. When these physiological function or processes become abnormal, a variety of diseases will appear, such as tumor, inflammation, some neurodegenerative diseases, and so on. Therefore, the proteasome has been considered to be a very potential novel target for antitumor drugs. Peptide boronic compound of bortezomib (PS-341) was the first listed proteasome inhibitor approved by FDA, clinically used for the treatment of multiple myeloma. Since then, the research of peptide boronic proteasomes is highly valued. As the research of peptide proteasome inhibitors moves towards increasing sophistication, it is found that peptide boronic compounds are accompanied by a lot of disadvantages such as laggard synthetic process, poor metabolic stability, narrow antitumor spectra, severe toxic side effects, highlighted drug resistance and so on. Therefore, novel proteasome inhibitors are urgent to be found.